Aarkstore Enterprise – Innovations in Oral Solid Drug Delivery: -Aarkstore Enterprise Market Research

Innovations in Oral Solid Drug Delivery: Advances in nanotechnology, controlled formulations & peptide delivery

Table of Contents :  

Innovations in oral solid drug delivery
Executive summary 18
Market overview, dynamics and outlook 18
Advances in nanotechnology 19
Innovations in transitioning injectables to oral delivery 20
Advances in delayed & controlled release delivery 21
Advances in oral prodrug delivery 22
Advances in taste masking technologies 23
Innovative companies 24
Chapter 1 Market overview, dynamics and outlook 28
Summary 28
Market overview 29
Market dynamics 31
Key indications 33
Key trends 38
Nanomedicine 38
Transitioning from injectables 39
Prodrugs 40
Chrono release 41
ODT 41
OSF 42
Funding issues 42
Poor patient compliance 42
Injections 42
Poor absorbption 42
Pediatric 43
Geriatric 43
Solubility and variable absorption 43
Reduction of side effect profiles 44
Non-invasive protein delivery 45
Transition from injectables to preferred route of oral drug delivery 45
Directed delivery and delayed delivery to reduce side effect potential 46
Formulation technologies for poorly soluble compounds 46
Taste masking for pediatric and geriatric formulations 47
Competitive landscape 48
Conclusions and key findings 50
Chapter 2 Advances in nanotechnology 56
Summary 56
Introduction 57
Nanotechnology platforms with application for oral drug delivery 59
Self-Emulsifying Controlled Release Tablet system (SECRET) 59
Technology 59
Application 59
Biotransport nanomedicine technology 60
Technology 60
Application 60
Nanobodies 61
Technology 61
Application 61
NanoDel nanoparticles 62
Technology 62
Application 62
P-gpMask 63
Technology 63
Application 64
NanoDRY and NanoCOAT 64
Technology 64
Application 64
Solumer 67
Technology 67
Application 67
Nanocells 69
Technology 69
Application 70
Polymeric Nano-Delivery System (PNDS) 70
Technology 70
Application 71
FluidCrystal NP Oral nanoparticles 71
Technology 71
Application 72
CaP Technology and BioOral 72
Technology 72
Application 73
Nab Technology and Protospheres 73
Technology 73
Application 73
NanoCrystal Technology 74
Technology 74
Application 74
Bioral 75
Technology 75
Application 75
Squalenoyl nanoparticles 76
NanoMega 76
NOD Pharmaceutical 76
Chapter 3 Innovations in transitioning injectables to oral delivery 80
Summary 80
Introduction 81
Drivers 81
Patient acceptability & compliance 81
Cost savings 81
Restraints 82
Advances in injectable delivery 82
Challenges of oral drug delivery 83
Technologies used in oral drug delivery of peptides and proteins 84
Enzyme inhibitors 84
Permeation enhancers 85
Mucoadhesives 85
Encapsulation technologies 85
M-cell targeting 86
Competitive landscape 86
Osteoporosis and other bone related conditions 88
Calcitonin 88
Current therapies & market landscape 89
Oral products in development 91
Parathyroid hormone 94
Current therapies & market landscape 94
Oral products in development 96
Combined oral calcitonin and PTH approaches 97
Bisphosphonates 97
Current therapies & market landscape 97
Novel oral products in development 99
Diabetes and other metabolic diseases 104
Oral insulin 104
Oramed Pharmaceuticals 104
Biocon Ltd 105
Emisphere Technologies 105
Diabetology 106
NOD Pharmaceuticals 106
Access Pharmaceuticals 107
NanoMega Medical Corporation 107
Biodel Inc 108
Metabolic Pharmaceuticals Ltd 108
Glucagon-like peptide-1 (GLP-1) and GLP-1 analogs 108
Oral GLP-1 & GLP-1 analogs 110
Obesity 114
Alzheimer’s and other CNS conditions 115
Oligotropin 115
Endometriosis and prostate cancer 115
Leuprolide 115
Cardiovascular 116
Angiotensin analogs 116
Innovative approaches to oral vaccine development 118
Mucosis B.V. 119
Plug-and-Play Technology 119
GEM Particles 119
Mimopath 119
Ondek Pty Ltd 120
Helicobacter pylori Platform Technology (HPPT) 120
Infexion 121
Kancer 121
Immune Solutions 121
Liporale 122
Chapter 4 Advances in delayed & controlled release delivery 124
Summary 124
Introduction 125
Types of controlled release systems 125
Sustained release 125
Pulsatile release 125
Modified drug delivery 126
Fast disintegrating technologies 126
Pediatric formulations – ODT 126
Schizophrenia and bipolar disorder – ODT 127
Alzheimer’s disease – ODT 128
Parkinson’s disease – ODT 129
Anxiety and panic disorder – ODT 129
Major depressive disorder – ODT 130
Nausea and vomiting – ODT 131
Migraine – ODT 131
Autism – ODT 132
GERD and gastroparesis – ODT 133
Release control mechanisms 135
Zero order 135
Congestive heart failure and hypertension – sustained release 135
Pain – sustained release 138
ADHD – sustained release 141
Multiple sclerosis – sustained release 141
Muscle relaxant – sustained release 142
Parkinson’s disease – sustained release 144
Depression – sustained release 144
Binary 147
Diabetes type 2 – combination products 147
Hypertension – combination products 149
Other 150
Biphasic release of drugs 150
Asthma – biphasic release 151
Pain – biphasic release 151
ADHD – biphasic release 152
Hypertension – biphasic release 152
Positioned 153
Parkinson’s disease – positioned biphasic release 154
Insomnia – positioned biphasic release 155
Spasticity – positioned biphasic release 156
GERD – positioned release 156
Diabetes type 2 – positioned extended release 157
Hot flashes – positioned extended release 157
Pain – positioned extended release 158
GERD – positioned extended release 158
Parkinson’s disease – positioned extended release 158
Others 159
Accelerated 159
Timed 159
Multiple pulse 160
Targeted delivery to the colon 160
Ulcerative colitis, gastroenteritis – targeted colon release 161
Nutraceutical – targeted colon release 162
Polysaccharide colon selective 163
COLAL technology 163
Chrono release 164
Rheumatoid arthritis – chrono release 165
Severe asthma – chrono release 166
Polymyalgia rheumatica – chrono release 166
Insomnia – chrono release 166
Sublingual formulations 167
Formulations to counteract opiate or psychostimulant abuse 167
Trigger-Lock 168
OraGuard 169
NanoDRY and NanoCOAT 170
ORADUR 170
Aversion Technology 171
Egalet ADPREM 172
DETERx 173
Avert 174
Strategic alliances 174
Chapter 5 Advances in oral prodrug delivery 178
Summary 178
Introduction 179
Classification based on site of conversion to active drug 181
Classification based on chemical linkages or promoiety/carriers that attach to
the active drug 182
Classification based on the deficiency in the active drug 183
Classification based on carrier-linked or bioprecursor categories 183
Applications of prodrug technology 185
Reducing side effect profile 185
Introducing site specificity – colon 185
Taste masking applications 186
Marketed products and market share 186
Antiviral prodrugs 186
Oseltamivir 186
Valaciclovir 187
Valganciclovir 189
Famciclovir 190
Anticancer prodrugs 191
TS-1 192
Cardiovascular prodrugs 194
ACE inhibitors 194
Angiotensin II receptor antagonists 194
HMG Co A reductase inhibitors 195
Respiratory prodrugs 195
Bambuterol 195
CNS prodrugs 195
Lisdexamfetamine 195
Late and early stage development product formulations 197
Improving oral bioavailability/reducing toxicity of older marketed injectable drugs 197
Antiviral prodrugs 197
Cidofovir 197
Vidarabine 200
Zanamivir 200
Anticancer prodrugs 201
Triciribine 201
Camptothecin 202
Gemcitabine 204
Docetaxel 206
Methotrexate 208
Aimpila 210
FAP activated ultra-smart prodrug cytotoxic agent 211

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Innovations in Oral Solid Drug Delivery and Advances in nanotechnology, controlled formulations & peptide delivery

This report concentrates on innovations in oral solid dose delivery systems (OSDDS) with an emphasis on the links between start up companies and academic collaborations. It deals with the impact of the difficult economic climate with the restriction on funding and opportunities for partnering projects.

Developments are assessed in relation to understanding the dynamics of the market. For instance the report discusses the loss of patent protection for blockbuster drugs peaking between 2007-2012, loss of patent protection for the first-generation of OSDDS in the last few years, the dearth of NCEs coming through the pipeline and puts new developments in the context of a market that is seeing a decline in its value in some therapeutic areas. It identifies the drivers for new OSDDS and the issues surrounding them.

A key theme is the transition of peptides and proteins from intravenous to oral delivery. The report looks at the competitive landscape, making reference to sales and market dynamics. A recurring theme is the reformulation of old generic drugs to get over inadequacies in the original drug for instance: low solubility, bioavailability, short duration of action, high side effect potential, poor stability, poor absorption following oral administration, bitter or unpleasant taste, narrow GI absorption window and inter- and intra-patient variability in absorption.

With a growing geriatric population and with people living longer much of the emphasis is on development of OSDDS drugs to more effectively treat diseases of an aging population such as Alzheimer’s disease, Parkinson’s disease, type 2 diabetes and obesity, osteoporosis, cancer and rheumatoid arthritis, etc. Often these treatments have side effects, problems with dosing and short duration of action or have to be administered by injection which reduces their acceptability.

Key features of this report

* Analysis of innovative platform technologies, companies and product development pipelines involved in transitioning injectable to oral drug delivery.
* Review of companies and technologies developing oral formulations of peptides and small proteins, highlighting stage of development, indications and competitive nature of the area.
* Providing an understanding of the specific problems involved in transitioning intravenous peptides to oral delivery and the mechanisms of crossing the GI mucosa, together with a review of approaches utilized.
* Analysis of sales data, growth rates, market share, generic entrants, new products for therapeutic areas in which the new products using the new technologies will compete.
* Assessment of market potential of the new osdds products in relation to the current market and competitors.

Scope of this report

* Get a comprehensive understanding of the range of new innovative osdds technologies and how they can overcome problems with the original active ingredient.
* Identify potential novel technologies which might allow you to overcome a problem with your own drug portfolio or which would allow you to extend your products’ franchise in the market place.
* Allow you to identify potential licensing opportunities or collaborations with innovative technology companies and assess the potential with respect to recent products commercialized.
* Allows you to identify which companies and which therapeutic areas are successful in gaining backing for their technologies and those that are not.
* Identify the time scales, hurdles and progress in developing new innovative technologies such as nanotechnologies/nanomedicines, oral peptides and proteins, new prodrugs and assess market factors affecting the developments and their success/failure.

Key Market Issues

* Asthe population ages and those elderly people live longer there is a greater need for better drugs which treat chronic conditions associated with aging such as Alzheimer’s disease, Parkinson’s disease, osteoporosis, rheumatoid arthritis, osteoarthritis, type 2 diabetes and obesity,cancer, hypertension and heart disease.
* The specific challenges in providing for mentally ill patients in which compliance is a problem is driving the demand for formulations which get over problems with swallowing difficulties, frequent dosing, variability in oral absorption or bioavailability,unacceptable side effect potential .
* The low numbers of new chemical entities approved annually (around 30 compared to 40-50 three decades ago), the record number of blockbuster drugs becoming generic up to 2012 and the first-generation delayed-release products losing patent protection is depressing the sales value in certain billion dollar therapy markets.

Key findings from this report

* The development of oral peptide hormones is a highly competitive area with many companies developing oral versions of the same peptide and these products will have to compete with new developments in inhaled peptides and very long-duration transdermal or sc depot products which are several years ahead of oral formulations.
* The failure of Exubera (inhaled insulin) has had a knock on effect on the development of new oral insulins with investors seeing oral insulins as being more risk prone and in addition the issues encountered with some oral insulins has meant that some companies are no longer considering this area a key focus.
* Many dds companies have switched their development focus to new oral GLP-1 analogs for the treatment of type 2 diabetes and obesity in the light of Byetta’s success but these oral products are several years behind the development of new long-acting transdermal, injectable and inhaled GLP-1 analogs .
* Generic nasal calcitonin products have depressed the value of second-generation nasal preparations which are still patent protected thus this does not bode well for prices achievable for oral salcatonin products which are nearing the market as they have to offer better therapeutic outcomes in order to achieve higher prices and ultimately market share.

Key questions answered

* What oral peptide products have the greatest growth potential and how far along the development path have they reached?
* What are the strategies employed by brand leaders to protect their franchise in the $10 billion US antiepileptic market in the face of recent generic competition?
* How has the failure of Exubera (inhaled insulin) affected the oral insulin developments and oral peptides in general?
* What are the main diseases and how advanced are the oral peptide and protein formulations?
* How successful is prodrug technology in terms of drug development and what are the latest developments?
* What innovative companies and platform technologies are attracting investment and collaboration agreements?

Nanotechnology ? Just What the Doctor Orders!

What if you were terminally ill and your doctor informed you that the venom from a snail could save your life?

What if the technology was available to produce a non-addictive painkiller that was thousands of times more potent than any morphine based product available today?

What if nanotechnology could provide the method of administering these potentially life-saving, pain elimination medicines within the near future? Would you be willing to support its advancement?

Well, nanotechnology is rapidly taking the “what if” out of just such medical conundrums. Biochemists, working in close liaison with nano-scientists, have discovered that the highly lethal venom contained in cone snails, which are found in coastal waters near coral reefs, can be extracted and, when administered via nanotechnologic methods, can potentially be used as a safe and effective alternative to highly addictive morphine-based medications.

Nanotechnology initiative programs are leading the highly competitive worldwide race in mining and providing a conduit for administering spiral snail toxins (known as conotoxins) and are developing methods of administering this peptide in a safe and positive manner.

Changes to the ion channels in human cells are directly responsible for a myriad of health disorders. Ion channels, which traditionally allow only calcium and potassium through their highly specific filtering system, can now be treated with toxins that have the ability to deactivate these channels. However, in the past, administration of these life altering conotoxins has offered a bit of a challenge to biology experts. That is, until now. This is where nanotechnology, with its innate ability to connect quantum dots, has provided a viable method of probing and infiltrating the cells in order to safely administer life altering drugs.

Due to its ability to specifically target finite and defined cells, nano-quantum dot technology provides the wherewithal to deliver conotoxins to targeted areas. Quantum dot, a nano-scale crystalline structure, is being investigated as a method of introducing medicine to specific areas of the body where the crystals act as probes that are able to track and report on antibodies, any viral activity, proteins in the area and even DNA composition.

By a system of imaging, this biochemistry and nanotechnology combination allows scientists and medical personnel alike to monitor the progression of the administered conotoxins within the body and allow the manipulation of toxin released at the designated sites.

Conotoxins have been proven as effective early detection and treatment methods for small cell lung cancer and for promoting anti-seizure treatment in epileptics. In addition, some success has been shown in treating patients who have suffered spinal cord injury, re-activating cells damaged due to oxygen deprivation and in treating clinical depression, irregular heart rhythms and some instances of urinary incontinence. Nanotechnology plays a vital role in the success of administering this innovative treatment by providing a safe and non-invasive method of administering treatment while reducing the risk of rejection by the body.

The possibility of advanced medical treatments when biochemistry, medicine and nanotechnology work in conjunction with one another is limitless.

Nanotechnology research has showed some promise in treatment of aging-related tissue degeneration in humans. With its in- vivo therapy, nanotechnology is credited with repairing degraded components of human DNA which significantly counterbalances and, in some cases, actually corrects the effects of common crippling age-related afflictions such as arthritis, osteoporosis and other debilitating diseases.